PE20160029A1 - Derivados de benzimidazol como inhibidores de bromodominio - Google Patents
Derivados de benzimidazol como inhibidores de bromodominioInfo
- Publication number
- PE20160029A1 PE20160029A1 PE2015002375A PE2015002375A PE20160029A1 PE 20160029 A1 PE20160029 A1 PE 20160029A1 PE 2015002375 A PE2015002375 A PE 2015002375A PE 2015002375 A PE2015002375 A PE 2015002375A PE 20160029 A1 PE20160029 A1 PE 20160029A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- inhibitors
- bromodominium
- benzimidazole derivatives
- dimethylisozaxol
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 229940058303 antinematodal benzimidazole derivative Drugs 0.000 title 1
- 150000001556 benzimidazoles Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 abstract 2
- 101710126815 Bromodomain-containing protein 4 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 108091005575 Bromodomain-containing proteins Proteins 0.000 abstract 1
- 102000001805 Bromodomains Human genes 0.000 abstract 1
- -1 cyclopropylmethylamino Chemical group 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente invencion se relaciona con compuestos quimicos que pueden actuar como inhibidores, o modular de alguna otra forma, la actividad de una proteina que contiene bromodominio, incluyendo de una proteina 4 que contiene bromodominio (BRD4) y con composiciones y formulaciones que contienen dichos compuestos, asi como metodos para realizar dichos compuestos. Los compuestos incluyen compuestos de Formula (I), en donde: R1a y R1b son alquilo C1-6, etc. R2a y R2b son H o halo, R3 es -C(O) ORA, etc. R4a y R4b es hidrogeno, etc. R5 es -C(O) ORA, etc. Ra es H, alquilo C1-10, etc. Compuestos preferidos son: N-Ciclopentil-2-(ciclopropilmetilamino)-6-(3,5-dimetilisozaxol-4-il)-1H-benzo[d] imidazol-4-sulfonamida; N- Ciclopentil-6-(3,5- dimetilisozaxol-4-il)-2-(3-metoxipropilamino)-1H-benzo[d] imidazol-4-sulfonamida
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361821612P | 2013-05-09 | 2013-05-09 | |
| US201361826912P | 2013-05-23 | 2013-05-23 | |
| US201361860229P | 2013-07-30 | 2013-07-30 | |
| US201461951347P | 2014-03-11 | 2014-03-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160029A1 true PE20160029A1 (es) | 2016-02-14 |
Family
ID=50897952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015002375A PE20160029A1 (es) | 2013-05-09 | 2014-05-08 | Derivados de benzimidazol como inhibidores de bromodominio |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US20160075695A1 (es) |
| EP (1) | EP2994469B1 (es) |
| JP (1) | JP6049942B2 (es) |
| KR (1) | KR101761049B1 (es) |
| CN (1) | CN105324379B (es) |
| AP (1) | AP2015008869A0 (es) |
| AR (1) | AR096246A1 (es) |
| AU (1) | AU2014262622B2 (es) |
| BR (1) | BR112015028017A2 (es) |
| CA (1) | CA2911408C (es) |
| CL (1) | CL2015003280A1 (es) |
| CR (1) | CR20150639A (es) |
| EA (1) | EA029091B1 (es) |
| ES (1) | ES2710120T3 (es) |
| MD (1) | MD4592B1 (es) |
| MX (1) | MX2015015478A (es) |
| NZ (1) | NZ713718A (es) |
| PE (1) | PE20160029A1 (es) |
| PH (1) | PH12015502534A1 (es) |
| PT (1) | PT2994469T (es) |
| SG (1) | SG11201509220XA (es) |
| TW (1) | TWI527811B (es) |
| UA (1) | UA112618C2 (es) |
| UY (1) | UY35559A (es) |
| WO (1) | WO2014182929A1 (es) |
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| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
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2014
- 2014-05-07 TW TW103116235A patent/TWI527811B/zh active
- 2014-05-08 MD MDA20150121A patent/MD4592B1/ro not_active IP Right Cessation
- 2014-05-08 BR BR112015028017A patent/BR112015028017A2/pt not_active Application Discontinuation
- 2014-05-08 MX MX2015015478A patent/MX2015015478A/es unknown
- 2014-05-08 AP AP2015008869A patent/AP2015008869A0/xx unknown
- 2014-05-08 NZ NZ713718A patent/NZ713718A/en not_active IP Right Cessation
- 2014-05-08 WO PCT/US2014/037344 patent/WO2014182929A1/en not_active Ceased
- 2014-05-08 CN CN201480035623.0A patent/CN105324379B/zh active Active
- 2014-05-08 KR KR1020157034918A patent/KR101761049B1/ko active Active
- 2014-05-08 SG SG11201509220XA patent/SG11201509220XA/en unknown
- 2014-05-08 AU AU2014262622A patent/AU2014262622B2/en active Active
- 2014-05-08 CA CA2911408A patent/CA2911408C/en active Active
- 2014-05-08 PT PT14729182T patent/PT2994469T/pt unknown
- 2014-05-08 US US14/787,374 patent/US20160075695A1/en not_active Abandoned
- 2014-05-08 EA EA201591965A patent/EA029091B1/ru not_active IP Right Cessation
- 2014-05-08 PE PE2015002375A patent/PE20160029A1/es not_active Application Discontinuation
- 2014-05-08 ES ES14729182T patent/ES2710120T3/es active Active
- 2014-05-08 US US14/273,147 patent/US9458145B2/en active Active
- 2014-05-08 EP EP14729182.7A patent/EP2994469B1/en active Active
- 2014-05-08 JP JP2016513078A patent/JP6049942B2/ja active Active
- 2014-05-09 UY UY0001035559A patent/UY35559A/es not_active Application Discontinuation
- 2014-05-09 AR ARP140101893A patent/AR096246A1/es unknown
- 2014-08-05 UA UAA201510960A patent/UA112618C2/uk unknown
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2015
- 2015-11-05 PH PH12015502534A patent/PH12015502534A1/en unknown
- 2015-11-09 CL CL2015003280A patent/CL2015003280A1/es unknown
- 2015-12-04 CR CR20150639A patent/CR20150639A/es unknown
-
2016
- 2016-08-17 US US15/239,422 patent/US10017501B2/en active Active
-
2018
- 2018-06-06 US US16/001,832 patent/US20180282316A1/en not_active Abandoned
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